• Title/Summary/Keyword: Antiproliferative activity

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Effects of Hypobaric Conditions on Apoptosis Signalling Pathways in HeLa Cells

  • Arican, Gul Ozcan;Khalilia, Walid;Serbes, Ugur;Akman, Gizem;Cetin, Idil;Arican, Ercan
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.12
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    • pp.5043-5047
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    • 2014
  • Nowadays increasing effectiveness in cancer therapy and investigation of formation of new strategies that enhance antiproliferative activity against target organs has become a subject of interest. Although the molecular mechanisms of apoptosis can not be fully explained, it is known that cell suicide program existing in their memory genetically is activated by pathophysiological conditions and events such as oxidative stress. Low pressure (hypobaric) conditions that create hypoxia promote apoptosis by inhibiting cell cycling. In this study, determination of the effects of fractional hypobaric applications at different times on HeLa cells at cellular and molecular levels were targeted. Experiments were carried out under hypobaric conditions (35.2 kPa) in a specially designed hypobaric cabin including 2% $O_2$ and 98% N. Application of fractional hypobaric conditions was repeated two times for 3 hours with an interval of 24 hours. At the end of the implementation period cells were allowed to incubate for 24 hours for activation of repair mechanisms. Cell kinetic parameters such as growth rate (MTT) and apoptotic index were used in determination of the effect of hypobaric conditions on HeLa cells. Also in our study expression levels of the Bcl-2 gene family that have regulatory roles in apoptosis were determined by the RT-PCR technique to evaluate molecular mechanisms. The results showed that antiproliferative effect of hypobaric conditions on HeLa cells started three hours from the time of application and increased depending on the period of exposure. While there was a significant decrease in growth rate values, there was a significant increase in apoptotic index values (p<0.01). Also molecular studies showed that hypobaric conditions caused a significant increase in expression level of proapoptotic gene Bax and significant decrease in antiapoptotic Bfl-1. Consequently fractional application of hypobaric conditions on HeLa cell cultures increased both antiproliferative and apoptotic effects and these effects were triggered by the Bax gene.

Volatile Compounds and Antiproliferative Effects of Dendropanax morbifera on HepG2 Cells (황칠나무의 휘발성 화합물 분석 및 HepG2 세포의 증식 억제 효과)

  • Yang, Seun-Ah;Garcia, Coralia V.;Lee, Ji-Won
    • Journal of Life Science
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    • v.27 no.5
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    • pp.561-566
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    • 2017
  • Dendropanax morbifera Lev. is known in Korea for its golden sap and medicinal properties. The many biological activities of the leaf and stem extracts suggest that this tree could be a valuable source of medicinal compounds for the treatment of various ailments such as dermatitis, migraines, dysmenorrhea, muscle pain, and infectious diseases. However, there is little information on the composition and biological activity of the volatile fraction of D. morbifera. Therefore, in this study, the volatile compounds in leaves, stems, and sap of D. morbifera were isolated using solvent and supercritical fluid extraction (SFE), and analyzed by gas chromatography/mass spectrometry to reveal their chemical composition and identify potential compounds of interest. Fifteen compounds were identified in the leaf extracts, whereas 29 and 3 compounds were identified in the stem and sap extracts, respectively. The volatile profiles obtained using solvent and SFE differed. Esters and aromatic hydrocarbons predominated in the solvent extract of leaves and SFE extract of stems, whereas the solvent extract of stems and SFE extract of leaves contained terpenoids. Limonene, ${\alpha}$-pinene, and ${\beta}$-myrcene were identified in the volatile extract of sap, with limonene representing 96.30% of the total peak area. In addition, the antiproliferative effects of the solvent extracts of leaves and stems were evaluated, revealing that these solvent extracts were particularly effective in decreasing the proliferation of HepG2 cells.

Comparison of proximate compositions, antioxidant, and antiproliferative activities between blueberry and Sageretia thea (Osbeck) M.C.Johnst fruit produced in Jeju Island (제주산 블루베리와 상동열매의 일반성분, 항산화 및 항증식 활성 비교)

  • Ko, Gyeong-A;Koh, So Yae;Ryu, Ji-yeon;Cho, Somi Kim
    • Journal of Applied Biological Chemistry
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    • v.60 no.2
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    • pp.161-171
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    • 2017
  • This study was aimed to evaluate and compare the proximate composition, antioxidant and antiproliferative activities of Sageretia thea (Osbeck) M.C.Johnst (S. thea) fruit and blueberry. The calorific value, crude protein, crude fat, crude ash, and carbohydrate were higher in S. thea fruit than in blueberry. S. thea fruit and blueberry have different profile of free sugars, in which amounts of fructose, glucose, and maltose were much higher in S. thea fruit than in blueberry. The methanol extracts of S. thea fruit contain higher amounts of total polyphenol and anthocyanin compared to those of blueberry extracts. In additions, 2,2-diphenyl-1-picrylhydrazyl (DPPH), alkyl, and 2,2'-azinobis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) radical scavenging activities are greater in S. thea fruit extracts. Ethyl acetate fractions and n-butanol fractions of S. thea fruit and blueberry show the most potent scavenging activity in DPPH-, alkyl-, and ABTS-radical scavenging assay. The ethyl acetate fractions of S. thea fruit and blueberry are the richest fraction in polyphenol contents while the n-butanol fractions of those are the highest fraction in anthocyanin contents. Furthermore, both S. thea fruit and blueberry extracts protect human dermal fibroblast cells against a $H_2O_2$-induced oxidative stress. The antiproliferative activities of n-hexane and chloroform fraction from S. thea fruit and blueberry were observed in AGS human gastric cancer and MDA-MB-231 human breast cancer cells. Therefore, our results suggest for the first time that the antioxidant and antiproliferative activities of S. thea fruit is comparable to that of blueberry and the nutritional value of the former is even superior to that of the latter.

Design, Synthesis, and Preliminary Cytotoxicity Evaluation of New Diarylureas and Diarylamides Possessing 1,3,4-Triarylpyrazole Scaffold

  • Choi, Won-Kyoung;El-Gamal, Mohammed I.;Choi, Hong-Seok;Hong, Jun-Hee;Baek, Dae-Jin;Choi, Ki-Hang;Oh, Chang-Hyun
    • Bulletin of the Korean Chemical Society
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    • v.33 no.9
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    • pp.2991-2998
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    • 2012
  • A series of new diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was synthesized and their in vitro antiproliferative activities against A375P human melanoma cell line and NCI-60 cell line panel were tested. Compounds 9, 11, 12, 14, and 17-21 showed superior potency against A375P to Sorafenib. Over the NCI-60 cancer cell line panel, compound 14 possessing a methoxy group, amide linker, and 4-chloro-3-(trifluoromethyl)phenyl terminal ring showed the highest potency and broad-spectrum anticancer activity. Compound 13 showed high selectivity towards leukemia subpanel over other cancer types.

Anti-proliferative and Apoptosis Inducing Effect of Momordin I on Oral Carcinoma (KB) Cells

  • Seo, Kyeong-Seong;Kim, Jeong-Hee;Kim, Yeo-Gab
    • International Journal of Oral Biology
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    • v.32 no.3
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    • pp.113-118
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    • 2007
  • Treatment of oral cancers with chemotherapeutic agents become evaluated as an effective method to reduce cancer cell proliferation. Anti-proliferative and anti-oral cancer activities of momordin I on oral cancer cells were evaluated in this study. Momordin I was originally purified from a natural product, Ampelopsis radix and showed the antiproliferative activity against oral carcinoma, KB cells. Obtained $IC_{50}$ value was approximately $10.4{\mu}g/ml$. Time-and dose-dependent chromosomal DNA fragmentations were observed in momordin I-treated KB cells. Flow cytometry analysis showed time-dependent apoptotic cell appearance after treatment of momordin I. Approximately 18.6% apoptotic cells were observed at 72 hours after $20{\mu}g/ml$ of momordin I treatment. These observation were consistent with the results obtained in DNA fragmentation analysis. These data suggest that momordin I has anti-proliferative effect and induces cell death in KB cells through apoptosis.

Chemical Constituents from the Aerial Parts of Bupleurum falcatum L. and Biological Evidences

  • Tung, Nguyen Huu;Uto, Takuhiro;Morinaga, Osamu;Shoyama, Yukihiro
    • Natural Product Sciences
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    • v.21 no.2
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    • pp.71-75
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    • 2015
  • In this study, phytochemical investigation on the aerial parts of Bupleurum falcatum resulted in the isolation of fourteen compounds including three quinic acid derivatives (1 - 3), five flavonoids (4 - 8), three monoterpene glycosides (9 - 11), and three saikosaponins (12 - 14). Compound 1 was first isolated from nature and unambiguously determined to be 3-O-feruloyl 5-O-caffeoylquinic acid on the basis of the extensive spectroscopic evidence. Biological testing revealed that saikosaponin A (12) and saikosaponin D (13) showed moderate antiproliferative effects on HL-60 and HepG2 cancer cell lines.

Atractylodes japonica Rhizome Inhibits Cell Proliferation and Induces Apoptosis in vitro

  • Choi, Eun-Jeong;Kim, Gun-Hee
    • Food Science and Biotechnology
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    • v.18 no.4
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    • pp.1019-1021
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    • 2009
  • Antiproliferative activity of the ethanol extract of Atractylodes japonica rhizomes (AJEX) was investigated using methyl thiazolyl tetrazolium (MTT) assays with various cancer cell lines (HL-60, MCF-7, SK-Br-3, MDA-MB-453, HepG2, Hep3B, PC-3, LNCaP, MKN 28, MKN 45, and HT-29 cells). Gastric carcinoma cell lines were the most responsive in terms of cell proliferation. The $IC_{50}$ of MKN 28 and MKN 45 cells were 35.98 and 27.57 ${\mu}g/mL$, respectively. Moreover, gastric carcinoma cells exposed to AJEX underwent apoptosis, as determined by Annexin V binding assay. Compared to respective control level, exposure to the AJEX at each $IC_{50}$ concentration resulted in a remarkable increase in the shift of cell populations. Present results suggest that AJEX possess potential anticancer properties.

CHEMOPREVENTION OF MAMMARY CARCINOGENESIS BY SYNTHETIC ANALOG OF VITAMIN D5.

  • Mehta, Rajendra G.;Hussain, Erum;Moriarty, Robert M.;Mehta, Rajeshwari R.;Das Gupta, Tapas K.
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.10a
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    • pp.52-53
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    • 2001
  • In order for vitamin D to be active, it needs to get metabolized to 1, 25 (OH)$_2$D3. This active metabolite of vitamin D induces epithelial cell differentiation and is antiproliferative. However, at the efficacious concentration, the natural ligand for VDR is hypercalcemic and toxic to cells. Therefore, numerous analogs have been synthesized with the hope of generating a compound that retains vitamin D activity and is non-toxic.(omitted)

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CHEMOPREVENTION OF MAMMARY CARCINOGENESIS BY SYNTHETIC ANALOG OF VITAMIN D5.

  • Mehta, Rajendra G.;Hussain, Erum;Moriarty, Robert M.;Mehta, Rajeshwari R.;DasGupta, Tapas K.
    • Proceedings of the Korean Society of Toxicology Conference
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    • 2001.10b
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    • pp.9-10
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    • 2001
  • In order for vitamin D to be active, it needs to get metabolized to 1, 25 (OH)$_2$D3. This active metabolite of vitamin D induces epithelial cell differentiation and is antiproliferative. However, at the efficacious concentration, the natural ligand for VDR is hypercalcemic and toxic to cells. Therefore, numerous analogs have been synthesized with the hope of generating a compound that retains vitamin D activity and is non-toxic.(omitted)

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Apoptosis Inducing Effects of 6-Methoxydihydrosanguinarine in HT29 Colon Carcinoma Cells

  • Lee, Yong-Jin;Yin, Hu-Quan;Kim, Young-Ho;Li, Guang-Yong;Lee , Byung-Hoon
    • Archives of Pharmacal Research
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    • v.27 no.12
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    • pp.1253-1257
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    • 2004
  • 6-Methoxydihydrosanguinarine (6ME), a benzophenanthridine alkaloid derived from the methanol extracts of Hylomecon hylomeconoides, showed a dose-dependent effect at 1-10 ${\mu}M$ on causing apoptotic cell death in HT29 colon carcinoma cells $(IC_{50} = 5.0{\pm}0.2 {\mu}M)$. Treatment of HT-29 cells with 6ME resulted in the formation of internucleosomal DNA fragmentation. Treatment of the cells with 6ME caused activation of caspase-3, -8 and 9 protease and subsequent proteolytic cleavage of poly(ADP-ribose)polymerase. 6ME increased the expression of p53 and Bax and decreased the expression of Bid. These results indicate that p53 and proapoptotic Bcl-2 family proteins might participate in the antiproliferative activity of 6ME in HT29 cells.